Colesevelam hydrochloride

What is Colesevelam hydrochloride?

• Colesevelam hydrochloride is a bile acid sequestrant as an adjunct to diet and exercise to reduce elevated low-density lipoprotein cholesterol (LDL-C) in patients with primary hyperlipidemia as monotherapy and to improve glycemic control in adults with type 2 diabetes mellitus.

Colesevelam structure

What are the uses of this medicine?

Colesevelam hydrochloride is used as an adjunct to diet and exercise to:

• reduce elevated low-density lipoprotein cholesterol (LDL-C) in adults with primary hyperlipidemia.
• reduce LDL-C levels in boys and postmenarchal girls, 10 to 17 years of age, with heterozygous familial hypercholesterolemia (HeFH), unable to reach LDL-C target levels despite an adequate trial of diet and lifestyle modification.
• improve glycemic control in adults with type 2 diabetes mellitus.

Limitations of Use:

• Do not use for treatment of type 1 diabetes or for diabetic ketoacidosis.
• Not studied in Fredrickson Type I, III, IV, and V dyslipidemias.

How does this medicine work?

Primary Hyperlipidemia:

• Colesevelam (koe" le sev' e lam) is a large, highly positively charged anion exchange resin that binds to negatively charged anions such as bile acids (as well as other organic compounds and some medications).
• The binding of bile acids to colesevelam creates an insoluble compound that cannot be reabsorbed and is thus excreted in the feces.
• Bile acids ordinarily undergo extensive (>95%) enterohepatic recirculation, being secreted in bile, acting as fat solubilizing compounds in the upper intestine, and then being reabsorbed in the distal small bowel.
• Chronic loss of bile acids results in a contraction in the total bile acid pool.
• The liver compensates for this decrease by increasing bile acid synthesis, which directly competes with cholesterol synthesis resulting in a decrease in serum levels.
• Some of the decrease in serum cholesterol may also result from inhibition of fat absorption by the binding of bile acids to colesevelam.

Type 2 Diabetes Mellitus:

• The mechanism by which colesevelam hydrochloride improves glycemic control is unknown.

Who Should Not Use this medicine ?

This medicine cannot used in patients with:

• Serum TG concentrations >500 mg/dL
• History of hypertriglyceridemia-induced pancreatitis
• A history of bowel obstruction

What drug interactions can this medicine cause?

• Concomitant use of drugs with a narrow therapeutic index (e.g., cyclosporine), phenytoin, thyroid hormone replacement therapy, warfarin, oral contraceptives containing ethinyl estradiol and norethindrone, olmesartan medoxomil, and sulfonylureas (glimepiride, glipizide, glyburide) may decrease the exposure of these drugs. Administer these drugs 4 hours prior to colesevelam hydrochloride. For patients on warfarin, monitor International Normalized Ratio (INR) frequently during initiation then periodically.
• Concomitant use with colesevelam hydrochloride may increase the exposure of metformin extended release. Monitor patients' glycemic control.

Is this medicine FDA approved?

• Colesevelam was approved for use in the United States in 2000 and is currently used largely as an adjunctive therapy when statins or other lipid lowering agents result in an inadequate decrease in cholesterol levels.
• Colesevelam is also approved as an adjunct to diet and exercise to improve glycemic control in type 2 diabetes.

How should this medicine be used?

• Obtain lipid parameters, including serum triglyceride (TG) levels, before starting colesevelam hydrochloride.

Recommended dosage:

• The recommended dosage for adults and for boys and postmenarchal girls aged 10 to 17 years with primary hyperlipidemia is 3.75 grams daily.
• The recommended dosage for adults with type 2 diabetes mellitus is 3.75 grams daily.

Colesevelam hydrochloride should be taken as follows: Tablets:

• Take 6 tablets once daily or 3 tablets twice daily with a meal and liquid.

For Oral Suspension

• Take one packet once daily with a meal.
• To prepare, empty the entire contents of one packet into a glass or cup.
• Add 1 cup of water, fruit juice, or diet soft drinks.
• Stir well and drink.

Administration:

• Take colesevelam hydrochloride tablets with a meal and liquid.
• For patients with difficulty swallowing tablets, use colesevelam hydrochloride for oral suspension.
• To prepare, empty the entire contents of one packet into a glass or cup.
• Add 1 cup (8 ounces) of water, fruit juice, or diet soft drinks.
• Stir well and drink.
• Take colesevelam hydrochloride oral suspension with meals.
• Do not take colesevelam hydrochloride oral suspension in its dry form.
• Due to tablet size, colesevelam hydrochloride for oral suspension is recommended for use in the pediatric population.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 625 mg
• For Oral Suspension: 3.75 gram packet

This medicine is available in fallowing brand namesː

• Welchol

What side effects can this medication cause?

The most common side effects of this medicine include:

• constipation
• dyspepsia
• nausea

What special precautions should I follow?

• Colesevelam hydrochloride can increase TG. Hypertriglyceridemia can cause acute pancreatitis. Monitor lipids, including TG. Instruct patients to discontinue colesevelam hydrochloride and seek prompt medical attention if the symptoms of acute pancreatitis occur.
• Cases of bowel obstruction have occurred. Colesevelam hydrochloride is not recommended in patients with gastroparesis, other gastrointestinal motility disorders, and in those who have had major gastrointestinal tract surgery and who may be at risk for bowel obstruction.
• Colesevelam hydrochloride may decrease absorption of fat-soluble vitamins. Patients with a susceptibility to deficiencies of vitamin K (e.g., patients on warfarin, patients with malabsorption syndromes) or other fat-soluble vitamins may be at increased risk. Patients on oral vitamin supplementation should take their vitamins at least 4 hours prior to colesevelam hydrochloride.
• Colesevelam hydrochloride reduces gastrointestinal absorption of some drugs. Administer drugs with a known interaction at least 4 hours prior to colesevelam hydrochloride.
• Phenylalanine can be harmful to patients with PKU. Colesevelam hydrochloride for oral suspension contains phenylalanine, a component of aspartame.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Excessive doses of colesevelam hydrochloride may cause more severe local gastrointestinal effects (e.g., constipation).

Treatment of overdosage:

• In the event of an overdose, appropriate supportive treatment should be initiated.

Can this medicine be used in pregnancy?

• Limited available data on the use of colesevelam hydrochloride are insufficient to determine a drug-associated risk of major congenital malformations or miscarriage.

Can this medicine be used in children?

• The safety and effectiveness of colesevelam hydrochloride in pediatric patients with HeFH less than 10 years of age or in premenarchal females have not been established.
• The safety and effectiveness of colesevelam hydrochloride to improve glycemic control in pediatric patients with type 2 diabetes mellitus have not been established.

What are the active and inactive ingredients in this medicine?

Active Ingredient:

• COLESEVELAM HYDROCHLORIDE

Inactive Ingredients:

• PROPYLENE GLYCOL ALGINATE
• DIMETHICONE
• ASPARTAME
• CITRIC ACID MONOHYDRATE
• MEDIUM-CHAIN TRIGLYCERIDES
• MAGNESIUM TRISILICATE

Who manufactures and distributes this medicine?

Distributed by:

• Sun Pharmaceutical Industries, Inc.
• Cranbury, NJ

Packager: Ohm Laboratories, Inc.

What should I know about storage and disposal of this medication?

• Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F).
• Protect from moisture.
• Brief exposure to 40°C (104°F) does not adversely affect colesevelam hydrochloride tablets.

• Dailymed label info on Colesevelam hydrochloride
• FDA Colesevelam hydrochloride

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